Synthesis, Biological Evaluation and Docking Studies of Aurone Derivatives on Xanthine Oxidase Enzyme

Authors

  • KAMAL RULLAH Sekolah Tinggi Ilmu Farmasi Riau, Universitas Riau, Kampus Bina Widya, Km 12.5, Simpang Baru-Pekanbaru 28293, Indonesia
  • SAW PHIN KHYE Drugs and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, 50300 Kuala Lumpur, Malaysia
  • ANG SERENE Drugs and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, 50300 Kuala Lumpur, Malaysia
  • MOHD FADHLIZIL FASIHI MOHD ALUWI Drugs and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, 50300 Kuala Lumpur, Malaysia
  • LAM KOK WAI Drugs and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, 50300 Kuala Lumpur, Malaysia

Keywords:

Auron, xantin oksidase, dok, sintesis, biologi

Abstract

Inhibition of xanthine oxidase (XO) activity is an effective therapeutic approach for the treatment of diseases such as gout and hyperuricemia. Additionally, the use of XO inhibitors can further be extended to injury treatments such as ischemic reperfusion in various organs such as heart, liver and kidney. In this study, 7 aurone compounds were synthesized and tested on XO and compared with the positive control allopurinol. Compound 5e was identified as the most potent compound and was able to inhibit half of XO activity at 33.23 μM followed by compounds 5f and 5d at 210.22 μM and 302.0 μM, respectively. Finally, molecular docking study was conducted to understand the important binding interactions of the selected aurone with the active site of XO.  DOI : http://dx.doi.org./10.17576/JSKM-2018-1601-17

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Published

2018-02-27

Issue

Vol. 16 No. 1 (2018)

Section

Biomedical Science

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